Stereoselectivity of NCS-382 (cas 131733-92-1) binding to γ-hydroxybutyrate receptor in the rat brain

Add time:07/24/2019    Source:sciencedirect.com

γ-Hydroxybutyric acid (GHB), a naturally occurring metabolite of γ-aminobutyric acid (GABA), has been postulated to act both as a specific agonist of GHB receptors and as a weak GABAB receptor agonist. The racemic compound 6,7,8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylideneacetic acid (RS-NCS-382 (cas 131733-92-1)), the only available antagonist of GHB receptors, has been resolved in two enantiomers, R- and S-; the potency of the latter to displace 4-hydroxy [2-3-3H] butyric acid ([3H]GHB) and [3H]NCS-382 from GHB receptors, on one hand, and [3H]baclofen from GABAB receptors on the other was compared in rat brain homogenates. R-NCS-382 was found to be twice and 60 times more potent than the RS- and S-forms, respectively, in displacing [3H]GHB and 2 and 14 times, respectively, in displacing [3H]NCS-382 from GHB binding. Neither RS-NCS-382 nor its enantiomers inhibited [3H]baclofen binding up to a concentration of 1 mM. Our results demonstrate that R-NCS-382 is the enantiomer of RS-NCS-382 with higher affinity for GHB receptors.

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Next:Regional Fos-expression induced by γ-hydroxybutyrate (GHB): Comparison with γ-butyrolactone (GBL) and effects of co-administration of the GABAB antagonist SCH 50911 and putative GHB antagonist NCS-382 (cas 131733-92-1))